公开(公告)号：WO2019097101A1

公开(公告)日：2019-05-23

申请号：PCT/ES2018/070735

申请日：2018-11-14

Applicant: UNIVERSIDAD DE VALLADOLID

Inventor： ÁLVAREZ MIGUEL, Lucía ,  BARBERO SAN JUAN, Héctor ,  GARCÍA RODRÍGUEZ, Raúl ,  ÁLVAREZ GONZÁLEZ, Celedonio Manuel ,  MIGUEL SAN JOSÉ, Daniel ,  MARTÍN ALVAREZ, José Miguel

IPC: A61K51/04 ,  C07F13/00 ,  C07K14/765 ,  G01N33/52 ,  G01N33/68

CPC classification number: A61K51/0455 ,  A61K51/081

Abstract: La presente invención describe una novedosa metodología de funcionalización de proteínas mediante la incorporación de un fragmento metálico de Renio con alto rendimiento, dando lugar a iminopiridinas coordinadas que poseen tres grupos carbonilo en posición fac - que ofrecen bandas procedentes de la tensión del enlace CO en el espectro de infrarrojo (IR) en una zona donde las proteínas no muestran señal alguna, lo que permite una aplicación muy interesante desde el punto de vista de detección de moléculas de interés biológico.

公开(公告)号：WO2016046793A2

公开(公告)日：2016-03-31

申请号：PCT/IB2015057378

申请日：2015-09-25

Applicant: SOUTH AFRICAN NUCLEAR ENERGY ,  UNIV CAPE TOWN

Inventor： DRIVER CATHRYN HELENA STANFORD ,  ZEEVAART JAN RIJN ,  PARKER MOHAMED IQBAL ,  HUNTER ROGER

IPC: A61K51/04

CPC classification number: A61K51/1045 ,  A61K51/0474 ,  A61K51/0491 ,  A61K51/0497 ,  A61K51/065 ,  A61K51/081 ,  A61K51/088 ,  A61K51/121

Abstract: This invention relates new radiopharmaceutical conjugates for use in improved methods of diagnosis and treatment of cancer. The radiopharmaceutical conjugate comprises, in sequence: a metabolite that targets tumour cells, bound to a chelating agent capable of containing a radionuclide.bound to a linker capable of binding with an EPR agent in vitro or in vivo; or a chelating agent capable of containing a radionuclide, bound to a metabolite that targets tumour cells, bound to a linker capable of binding with an EPR agent in vitro or in vivo. The radiopharmaceutical conjugates of the present invention provide active and passive targeted radionuclide delivery systems that can help to improve the biodistribution and pharmacological toxicity of the radiopharmaceuticals used for the diagnosis and therapy of cancer.

Abstract translation: 本发明涉及用于癌症诊断和治疗的改进方法中的新的放射性药物缀合物。 放射性药物缀合物依次包含：靶向肿瘤细胞的代谢物，其与能够含有放射性核素的螯合剂结合，能够在体外或体内与EPR剂结合; 或能够含有与靶向肿瘤细胞的代谢物结合的放射性核素的螯合剂，其与能够在体外或体内与EPR剂结合的接头结合。 本发明的放射性药物缀合物提供主动和被动靶向的放射性核素递送系统，其可以帮助改善用于诊断和治疗癌症的放射性药物的生物分布和药理学毒性。

公开(公告)号：WO2012004384A2

公开(公告)日：2012-01-12

申请号：PCT/EP2011/061623

申请日：2011-07-08

Applicant: AFFIBODY AB ,  EKBLAD, Caroline ,  ABRAHMSÉN, Lars

Inventor： EKBLAD, Caroline ,  ABRAHMSÉN, Lars

IPC: C07K14/195

CPC classification number: C07K14/315 ,  A61K38/00 ,  A61K51/081 ,  C07K14/001 ,  C07K2319/21 ,  C07K2319/31 ,  C07K2319/50 ,  C07K2319/70 ,  Y02A50/473

Abstract: The present disclosure relates to a class of engineered polypeptides having a binding affinity for albumin. It also relates to new methods and uses that exploit binding by these and other compounds to albumin in different contexts, some of which have significance for treatment or diagnosis of disease in mammals including humans.

Abstract translation: 本公开涉及对白蛋白具有结合亲和力的一类工程化多肽。 它还涉及利用这些化合物和其他化合物在不同情况下与白蛋白结合的新方法和用途，其中一些对于哺乳动物包括人类中的疾病的治疗或诊断具有重要意义。

公开(公告)号：WO2010087612A1

公开(公告)日：2010-08-05

申请号：PCT/KR2010/000488

申请日：2010-01-27

Applicant: SNU R&DB FOUNDATION ,  JEONG, Jae Min ,  LEE, Myung Chul ,  CHUNG, June Key ,  LEE, Dong Soo

Inventor： JEONG, Jae Min ,  LEE, Myung Chul ,  CHUNG, June Key ,  LEE, Dong Soo

IPC: A61K51/08

CPC classification number: A61K51/081 ,  A61K51/0482

Abstract: The present invention is about bifunctional chelating agents (BCA) conjugated mannosyl human serum albumin (MSA) and its radioisotope labeled compounds for imaging immune system such as macrophages, Kupffer cells, reticuloendothelial system (RES), and lymphatic system. The present invention comprises BCA-MSA conjugates, their radiolabeled compounds, and kits for radiolabeing. The present invention improved radiolabeling procedure, showed higher lymphatic system uptake, and enabled image by positron emission tomography (PET).

Abstract translation: 本发明涉及双功能螯合剂（BCA）共轭甘露糖基人血清白蛋白（MSA）及其放射性同位素标记化合物，用于成像免疫系统如巨噬细胞，枯否细胞，网状内皮系统（RES）和淋巴系统。 本发明包括BCA-MSA缀合物，它们的放射性标记化合物和放射性试剂盒。 本发明改善放射性标记程序，显示较高的淋巴系统摄取，并通过正电子发射断层扫描（PET）实现图像。

公开(公告)号：WO2009129577A1

公开(公告)日：2009-10-29

申请号：PCT/AU2009/000508

申请日：2009-04-23

Applicant: THE AUSTRALIAN NATIONAL UNIVERSITY ,  STEPHENS, Ross, Wentworth ,  SENDEN, Timothy, John ,  KING, David, Wallace

Inventor： STEPHENS, Ross, Wentworth ,  SENDEN, Timothy, John ,  KING, David, Wallace

IPC: A61K51/06 ,  A61K49/12 ,  A61K49/14 ,  A61K49/16 ,  A61K51/08 ,  A61K51/10 ,  A61P35/00

CPC classification number: A61K51/1251 ,  A61K41/0095 ,  A61K51/06 ,  A61K51/08 ,  A61K51/081 ,  A61K51/10

Abstract: The present invention relates to a method for preparing a radiolabeled macromolecule, the method comprising contacting a macromolecule with a carbon encapsulated nanoparticle composite having a radioactive particulate core in an aqueous medium comprising a pH selected to promote short-range attractive forces between the nanoparticles and the macromolecule by attenuating repulsive electrostatic forces.

Abstract translation: 本发明涉及一种制备放射性标记的高分子的方法，该方法包括使高分子与含有放射性颗粒核的碳包覆的纳米颗粒复合物在水性介质中接触，所述水性介质包含选择的pH以促进纳米颗粒与所述纳米颗粒之间的短程吸引力 大分子通过衰减排斥静电力。

公开(公告)号：WO2003027148A1

公开(公告)日：2003-04-03

申请号：PCT/KR2002/001787

申请日：2002-09-19

Applicant: JEONG, Jae, Min ,  LEE, Jaetae

Inventor： JEONG, Jae, Min ,  LEE, Jaetae

IPC: C07K14/765

CPC classification number: A61K51/0491 ,  A61K47/643 ,  A61K51/081 ,  A61K51/088 ,  C07K14/765

Abstract: Disclosed are disulfide-reduced neogalactosyl serum albumin and use of its radiolabeled derivative for liver imaging. More particularly, the present invention relates to disulfide-reduced neogalactosyl serum albumin represented by the following Formula 1 and a method of preparing the same, as well as its radiolabeled derivative. Also, the present invention is concerned with a kit for liver imaging, which is capable of radiolabeling neogalactosyl human serum albumin. The radiolabeled compound according to the present invention has excellent stability as well as a high accumulation rate in liver, thereby allowing its application in liver imaging Formula (I), wherein, Ga1, L, A, n, and m are described in detail in the specification.

Abstract translation: 公开了二硫化物还原型新乳糖基血清白蛋白和其放射性标记衍生物用于肝脏成像。 更具体地，本发明涉及由下式1表示的二硫化物还原型新半乳糖基血清白蛋白及其制备方法及其放射性标记衍生物。 此外，本发明涉及能够放射性标记新乳糖基人血清白蛋白的用于肝脏成像的试剂盒。 根据本发明的放射性标记化合物在肝脏中具有优异的稳定性和高的蓄积率，从而允许其应用于肝脏成像。其中，Ga1，L，A，n和m在肝脏成像中的应用详细描述于 规格。

公开(公告)号：WO1996025956A2

公开(公告)日：1996-08-29

申请号：PCT/DE1996000267

申请日：1996-02-21

Applicant: DEUTSCHES KREBSFORSCHUNGSZENTRUM STIFTUNG DES ÖFFENTLICHEN RECHTS ,  SINN, Hannsjörg ,  MAIER-BORST, Wolfgang ,  SCHRENK, Hans-Hermann ,  STEHLE, Gerd

Inventor： DEUTSCHES KREBSFORSCHUNGSZENTRUM STIFTUNG DES ÖFFENTLICHEN RECHTS

IPC: A61K51/08

CPC classification number: A61K51/088 ,  A61K31/136 ,  A61K47/54 ,  A61K47/547 ,  A61K51/081

Abstract: A conjugate comprises an active substance and a compound with a binding site for metallic compounds. Also disclosed is a process for preparing such a conjugate and its use.

Abstract translation: 本发明涉及用活性成分和用于承载化合物的金属化合物的结合位点的缀合物。 本发明还涉及一种用于制造这种共轭和其使用的方法。

公开(公告)号：WO1992019213A2

公开(公告)日：1992-11-12

申请号：PCT/US1992003667

申请日：1992-05-01

Applicant: UNIVERSITY OF NEW MEXICO

Inventor： UNIVERSITY OF NEW MEXICO ,  BORN, Jerry, L. ,  ESHIMA, Dennis ,  MANN, Paul, L. ,  MATWIYOFF, Nicholas, A. ,  RHODES, Buck, A.

IPC: A61K0

CPC classification number: A61K49/16 ,  A61K47/6415 ,  A61K49/085 ,  A61K49/14 ,  A61K51/08 ,  A61K51/081 ,  A61K51/1033 ,  A61K51/1045 ,  A61K51/1087 ,  A61K2123/00

Abstract: Biomodulators, in conjuction with antibodies, tumor-specific agents or conjugates thereof, optionally linked to imaging-active moieties, can be administered to a host to enhance images thereof, e.g., NMR-, X-Ray- or radioimages, preferably by increasing aberrant tissue signal intensity.

Abstract translation: 结合抗体的生物调节剂，任选与成像活性部分连接的肿瘤特异性试剂或其缀合物可以施用于宿主以增强其图像，例如NMR-，X射线或放射线图像，优选通过增加异常 组织信号强度。

公开(公告)号：WO2012160450A2

公开(公告)日：2012-11-29

申请号：PCT/IB2012/050624

申请日：2012-02-13

Applicant: CONTANGO PARTNERS GROUP, INC. ,  SOBOLEV, Alexander, S. ,  ROSENKRANZ, Audrey, A. ,  JANS, David, A. ,  LUNIN, Vladimir, G.

Inventor： SOBOLEV, Alexander, S. ,  ROSENKRANZ, Audrey, A. ,  JANS, David, A. ,  LUNIN, Vladimir, G.

CPC classification number: A61K47/48269 ,  A61K41/0071 ,  A61K47/6415 ,  A61K47/642 ,  A61K47/6445 ,  A61K51/081 ,  A61K51/088

Abstract: The invention relates to a modular transport platform (MTP) for delivering active, diagnostic or research substances to predesigned intracellular compartments of target cells. The MTP includes functional modules within one molecule to accomplish one or more of the following: penetration of the modular transport platform into a target cell type, pH-dependent membrane disruption activity within the target cell, directed intracellular transport into preselected intracellular compartment, and delivery of a substance to be transported to the intracellular compartment. The modular transport platform includes the following modules: (1) a ligand module to target a specific receptor on the surface of the target cell; (2) an endosomolytic module that provides pH-dependent membrane disruption activity within the target cell; (3) an intracellular transport module to cause delivery of the MTP to a particular subcellular compartment; (4) a module for intracellular retention to ensure retention of the MTP within the subcellular compartment of the target cell; (5) a module for subcellular recognition; (6) a substance to be transported by the MTP; and (7) a carrier module for unifying the modules and coupling the modules with the transported substance.

Abstract translation: 本发明涉及用于将活性，诊断或研究物质递送到靶细胞的预先设计的细胞内区室的模块化转运平台（MTP）。 MTP包括一个分子内的功能模块，以实现以下一个或多个：模块化传输平台渗透到靶细胞类型中，靶细胞内的pH依赖性膜破坏活性，定向细胞内转运到预选的细胞内区室和递送 的物质被运送到细胞内隔室。 模块化运输平台包括以下模块：（1）靶靶细胞表面上特定受体的配体模块; （2）在靶细胞内提供pH依赖性膜破坏活性的内体分解模块; （3）细胞内转运模块，以使MTP递送至特定的亚细胞室; （4）用于细胞内保留的模块以确保MTP在靶细胞的亚细胞间隔内的保留; （5）用于亚细胞识别的模块; （六）中期计划运输的物质; 和（7）用于统一模块并将模块与输送的物质耦合的载体模块。

公开(公告)号：WO2012021045A3

公开(公告)日：2012-05-10

申请号：PCT/KR2011005994

申请日：2011-08-16

Applicant: NAT CANCER CT ,  KIM SEOK KI ,  KANG SE HUN ,  KIM SEO IL ,  KIM YOUNG SANG ,  BAEK NAM SUK ,  NOH JIN HEE

Inventor： KIM SEOK KI ,  KANG SE HUN ,  KIM SEO IL ,  KIM YOUNG SANG ,  BAEK NAM SUK ,  NOH JIN HEE

IPC: G01N33/60 ,  A61K51/00 ,  G01N33/52 ,  G21H5/00

CPC classification number: A61K51/081 ,  A61K49/0002 ,  A61K49/0021 ,  A61K49/0034 ,  A61K49/0056 ,  A61K49/006 ,  G01N33/534 ,  G01N2333/765

Abstract: The present invention relates to a sentinel lymph node marker comprising albumin to which a radioactive isotope, one or more dyes selected from near-infrared ray absorbing dyes, and a visible ray absorbing dye are coupled, a preparation method thereof, a kit for preparing the same for multi-mode imaging the sentinel lymph node, and a multi-mode imaging method of the sentinel lymph node using the same. The sentinel lymph node marker of the present invention has a long retention time at a lymph node and enables multi-mode imaging, and thus it is possible to precisely check the sentinel lymph node without a skin incision by ex vivo imaging through a near-infrared image and/or gamma ray image, and it is possible to precisely check the location of the sentinel lymph node with the naked eye when used in conjunction with surgery for removing the checked sentinel lymph node.

Abstract translation: 本发明涉及包含白蛋白的前哨淋巴结标记物，其中放射性同位素，一种或多种选自近红外线吸收染料和可见光吸收染料的染料偶联，其制备方法，用于制备 前哨淋巴结的多模式成像相同，前哨淋巴结的多模式成像方法也是如此。 本发明的前哨淋巴结标记物在淋巴结处具有较长的保留时间，能够实现多模式成像，因此可以通过近红外线的离体成像来精确检查前哨淋巴结，无需皮肤切口 图像和/或γ射线图像，并且当与用于移除检查的前哨淋巴结的手术结合使用时，可以用肉眼精确地检查前哨淋巴结的位置。